Activation and Delivery of Tetrazine-Responsive Bioorthogonal Prodrugs

Prodrugs, which remain inert until they are activated under appropriate conditions at the target site, have emerged as an attractive alternative to drugs that lack selectivity and show off-target effects. Prodrugs have traditionally been activated by enzymes, pH or other trigger factors associated w...

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Main Authors: Yayue Wang, Chang Zhang, Haoxing Wu, Ping Feng
Format: Article
Language:English
Published: MDPI AG 2020-11-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/25/23/5640
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spelling doaj-4f09ebdf249443a393cc056e8283fcdc2020-12-01T00:02:11ZengMDPI AGMolecules1420-30492020-11-01255640564010.3390/molecules25235640Activation and Delivery of Tetrazine-Responsive Bioorthogonal ProdrugsYayue Wang0Chang Zhang1Haoxing Wu2Ping Feng3Huaxi MR Research Center, Department of Nuclear Medicine, Frontiers Science Center for Disease-Related Molecular Network, West China Hospital, Sichuan University, Chengdu 610041, ChinaHuaxi MR Research Center, Department of Nuclear Medicine, Frontiers Science Center for Disease-Related Molecular Network, West China Hospital, Sichuan University, Chengdu 610041, ChinaHuaxi MR Research Center, Department of Nuclear Medicine, Frontiers Science Center for Disease-Related Molecular Network, West China Hospital, Sichuan University, Chengdu 610041, ChinaInstitute of Clinical Trials, West China Hospital, Sichuan University, Chengdu 610041, ChinaProdrugs, which remain inert until they are activated under appropriate conditions at the target site, have emerged as an attractive alternative to drugs that lack selectivity and show off-target effects. Prodrugs have traditionally been activated by enzymes, pH or other trigger factors associated with the disease. In recent years, bioorthogonal chemistry has allowed the creation of prodrugs that can be chemically activated with spatio-temporal precision. In particular, tetrazine-responsive bioorthogonal reactions can rapidly activate prodrugs with excellent biocompatibility. This review summarized the recent development of tetrazine bioorthogonal cleavage reaction and great promise for prodrug systems.https://www.mdpi.com/1420-3049/25/23/5640tetrazinebioorthogonal reactionprodrug activation
collection DOAJ
language English
format Article
sources DOAJ
author Yayue Wang
Chang Zhang
Haoxing Wu
Ping Feng
spellingShingle Yayue Wang
Chang Zhang
Haoxing Wu
Ping Feng
Activation and Delivery of Tetrazine-Responsive Bioorthogonal Prodrugs
Molecules
tetrazine
bioorthogonal reaction
prodrug activation
author_facet Yayue Wang
Chang Zhang
Haoxing Wu
Ping Feng
author_sort Yayue Wang
title Activation and Delivery of Tetrazine-Responsive Bioorthogonal Prodrugs
title_short Activation and Delivery of Tetrazine-Responsive Bioorthogonal Prodrugs
title_full Activation and Delivery of Tetrazine-Responsive Bioorthogonal Prodrugs
title_fullStr Activation and Delivery of Tetrazine-Responsive Bioorthogonal Prodrugs
title_full_unstemmed Activation and Delivery of Tetrazine-Responsive Bioorthogonal Prodrugs
title_sort activation and delivery of tetrazine-responsive bioorthogonal prodrugs
publisher MDPI AG
series Molecules
issn 1420-3049
publishDate 2020-11-01
description Prodrugs, which remain inert until they are activated under appropriate conditions at the target site, have emerged as an attractive alternative to drugs that lack selectivity and show off-target effects. Prodrugs have traditionally been activated by enzymes, pH or other trigger factors associated with the disease. In recent years, bioorthogonal chemistry has allowed the creation of prodrugs that can be chemically activated with spatio-temporal precision. In particular, tetrazine-responsive bioorthogonal reactions can rapidly activate prodrugs with excellent biocompatibility. This review summarized the recent development of tetrazine bioorthogonal cleavage reaction and great promise for prodrug systems.
topic tetrazine
bioorthogonal reaction
prodrug activation
url https://www.mdpi.com/1420-3049/25/23/5640
work_keys_str_mv AT yayuewang activationanddeliveryoftetrazineresponsivebioorthogonalprodrugs
AT changzhang activationanddeliveryoftetrazineresponsivebioorthogonalprodrugs
AT haoxingwu activationanddeliveryoftetrazineresponsivebioorthogonalprodrugs
AT pingfeng activationanddeliveryoftetrazineresponsivebioorthogonalprodrugs
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